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5-hydroxytryptamine hydrochloride is an indole derivative, called 5-HT hydrochloride. It is first found in serum, also known as serotonin. It widely exists in mammalian tissues, especially in the cerebral cortex and synapses. It is also an inhibitory neurotransmitter. White powder, soluble in water, stable under normal temperature and pressure, sealed in a dry and cool place, away from strong oxidants.
Its role in sleep is controversial: early studies showed that serotonin can promote sleep, but the final research paradigm has shifted to the wake-up function of serotonin. 5-hydroxytryptamine, as a neurotransmitter, can participate in various central nervous system activities and is a messenger of pleasure emotions, affecting almost every aspect of brain activity. With the rapid development of health products, 5-hydroxytryptamine is also increasingly used in health products. Nowadays, 5-hydroxytryptamine is widely used in many large health companies in Europe and America.
Some studies have shown that serotonin promotes sleep, but other studies have shown that serotonin producing neurons are most active when awake, when they release a large amount of serotonin. However, it is recognized that it is an important neurotransmitter. It plays a role in the brain, enabling us to feel happy and happy. Therefore, it is also called "happy neurotransmitter". It participates in a wide range of physiological functions of the human body, including regulation of brain memory, cognition, emotion, learning and addiction. The disorder of this system may lead to a variety of mental diseases, such as depression, schizophrenia, etc.
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Chemical Formula |
C10H13ClN2O |
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Exact Mass |
212 |
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Molecular Weight |
213 |
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m/z |
212 (100.0%), 214 (32.0%), 213 (10.8%), 215 (3.5%) |
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Elemental Analysis |
C, 56.48; H, 6.16; Cl, 16.67; N, 13.17; O, 7.52 |
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melting point 149 – 154 °C ( lit. ), Storage conditions 2-8 ° C, Solubility H2O: 17 mg / mL morphological powder, Color white to off-white, Water-soluble, Sensitive Light Sensitive & Hygroscopic, BRN 3570963, stable, but light-sensitive and hygroscopic. Incompatible with oxidizing agents. , InChIKeyMDIGAZPGKJFIAH-UHFFFAOYSA-N, Hazardous Mark Xn, Xi, Hazard, Hazard category code 20 / 21 / 22-36 / 37 / 38, Safety instructions 22-26-36, Transport number of dangerous goods UN2811, WGK Germany 3, RTECS NM2571000, F 3-8-10, HazardClass 6.1, Packing Group III.
5-hydroxytryptamine hydrochloride (CAS number 153-98-0), as the hydrochloride form of 5-hydroxytryptamine (5-HT), is a key compound in neuroscience, pharmacology, and biomedical research. Its molecular formula is C10H12N2O · HCl, with a molecular weight of 212.68. It is a white to off white crystalline powder at room temperature and is easily soluble in water (17 mg/mL) and acidic solutions.
1. Core tools for studying neurotransmitter function
5-HT hydrochloride is a standard reagent for studying the 5-HT neurotransmitter system. As an endogenous 5-HT receptor agonist, it simulates the signaling process of 5-HT under physiological conditions by activating 5-HT ₁ to 5-HT ₇ receptor subtypes. For example:
Identification of receptor subtypes: By adding different concentrations of 5-HT hydrochloride to neurons or transgenic cell lines cultured in vitro, changes in second messengers (such as cAMP and calcium ions) after receptor activation can be observed to clarify receptor functional characteristics.
Signal pathway analysis: By combining gene editing techniques such as CRISPR-Cas9, the regulatory effects of 5-HT binding to receptors on downstream protein kinases such as PKA and MAPK can be studied, revealing the molecular mechanisms of physiological processes such as emotions and sleep.
2. Model compounds for neurodevelopment and plasticity research
5-HT is involved in neural development and synaptic plasticity regulation during both embryonic and adult stages. 5-HT hydrochloride can be used for:
Neuronal differentiation induction: In vitro neural stem cell culture, the addition of 5-HT hydrochloride can promote its differentiation into 5-HTergic neurons, providing a model for studying neurodevelopmental diseases such as autism.
Observation of synaptic formation: Real time monitoring of changes in the number of neuronal synapses after treatment with 5-HT hydrochloride can be achieved through fluorescence labeling technology, revealing its relationship with learning and memory.
3. Inducing agents for disease model construction
In animal models, serotonin hydrochloride can induce specific pathological states:
Depression model: Chronic injection of low-dose serotonin hydrochloride can simulate the dysfunction of the 5-HT system in patients with depression and observe changes in animal behavior (such as prolonged immobility in forced swimming tests).
Migraine model: Local injection of 5-HT hydrochloride can activate the trigeminal vascular system, induce headache like behavior, and be used for screening anti migraine drugs.
Neuroscience: Regulators of Emotion, Sleep, and Cognition
1. The core medium of emotional regulation
The 5-HT system is the central hub for emotion regulation. 5-HT hydrochloride participates in:
Antidepressant mechanism: Selective 5-HT reuptake inhibitors (SSRIs, such as fluoxetine) alleviate depressive symptoms by blocking 5-HT transporters and increasing synaptic 5-HT concentration. 5-HT hydrochloride itself can serve as a control reagent for studying the effects of SSRI.
Anxiety and aggression: Abnormal 5-HT levels are associated with anxiety disorders and impulsive aggressive behavior. Animal experiments have shown that 5-HT hydrochloride can reduce 5-HT levels in aggressive mice and improve their social behavior.
2. Regulating factors of sleep wake cycle
5-HT participates in sleep regulation by activating 5-HT ₁ A and 5-HT ₂ C receptors:
Sleep promoting effect: After injecting 5-HT hydrochloride into the ventricles, it can shorten the latency period of sleep onset in rats and increase non rapid eye movement sleep (NREM) time.
Synchronization of circadian rhythm: 5-HT is involved in the regulation of the circadian rhythm of the hypothalamic suprachiasmatic nucleus (SCN), and 5-HT hydrochloride can be used to study the effect of photoperiod on sleep.
3. Neurochemical basis of cognitive function
5-HT affects cognitive function through the prefrontal cortex and hippocampus:
Learning and memory: 5-hydroxytryptamine hydrochloride can enhance the performance of spatial memory tasks (such as Morris water maze), and its effect depends on the activation of 5-HT ₄ receptors.
Attention and Decision making: Abnormal 5-HT levels are associated with Attention Deficit Hyperactivity Disorder (ADHD), and 5-HT hydrochloride can be used to study the impact of 5-HT on decision-making behavior.
1. Drug screening and mechanism of action research
5-HT hydrochloride is a key tool in the development of antidepressants, antipsychotics, and anti migraine drugs:
Receptor binding assay: Through radioligand binding assay, the affinity of candidate drugs to 5-HT receptors can be determined, and potential active molecules can be screened.
Functional activity assessment: At the cellular level, the regulatory effect of drugs on receptor function (such as excitatory, antagonistic, or allosteric regulation) is evaluated by detecting changes in cAMP or calcium ions induced by serotonin hydrochloride.
2. Research on drug metabolism and pharmacokinetics
5-HT transporter (SERT) is the target of SSRI drugs. 5-HT hydrochloride can be used for:
Transporter dynamics analysis: Determine the inhibition constant (Ki) of drugs on SERT through competitive inhibition experiments, and predict their in vivo efficacy.
Metabolic stability testing: Observe the metabolites of 5-HT hydrochloride in a liver microsomal incubation system to evaluate the induction or inhibition of drug metabolizing enzymes.
3. Toxicity assessment and safety pharmacology
Serotonin syndrome (SS) is a serious adverse reaction of 5-HT drug overdose or combination therapy. 5-HT hydrochloride can be used for:
Toxicity mechanism study: Through animal models, observe the induction of elevated body temperature, muscle spasms, and consciousness disorders by high-dose 5-HT hydrochloride, and reveal the pathological and physiological processes of SS.
Safety window determination: In vitro cytotoxicity tests, the half maximal inhibitory concentration (IC ₅₀) of serotonin hydrochloride is determined to provide reference for clinical drug safety.
Clinical application: a versatile approach from diagnosis to treatment
1. Diagnostic biomarkers for neurological and psychiatric disorders
Abnormal 5-HT system function is associated with various psychiatric disorders:
Biomarkers for depression: Detection of serotonin hydrochloride metabolites (such as 5-hydroxyindoleacetic acid, 5-HIAA) through lumbar puncture or cerebrospinal fluid testing can assist in the diagnosis of depression.
Migraine classification: 5-HT levels significantly decrease during migraine attacks, and serotonin hydrochloride testing can be used to distinguish migraine from other types of headaches.
2. Auxiliary methods for tumor treatment
5-HT has anti-tumor potential:
Direct inhibition of tumor growth: In vitro experiments have shown that 5-HT hydrochloride can induce apoptosis in colon cancer cells, and its effect depends on the activation of 5-HT ₁ D receptors.
Synergistic effect of immune regulation: 5-HT can enhance the cytotoxicity of natural killer (NK) cells, and its combination with immune checkpoint inhibitors may improve anti-tumor efficacy.
3. Innovative therapies for pain management
5-HT participates in pain signal transduction:
Neuropathic pain: 5-HT hydrochloride activates 5-HT ₇ receptors in the spinal dorsal horn, inhibits pain signal transmission, and provides a new target for the treatment of chronic pain.
Acute treatment of migraine: 5-HT receptor agonists (such as sumatriptan) are first-line drugs for acute migraine attacks, and their mechanism of action is similar to that of serotonin hydrochloride.
Industrial sector: Potential stocks for biotechnology and agricultural applications
1. Development of biosensors
5-HT detection is crucial in neuroscience research and clinical diagnosis. The electrochemical sensor based on 5-hydroxytryptamine hydrochloride can achieve:
Real time monitoring: By modifying the electrode surface, high-sensitivity detection of 5-HT levels in cerebrospinal fluid or blood can be achieved, which can be used for epilepsy seizure warning or depression efficacy evaluation.
Portable device: Combined with microfluidic technology, a miniaturized 5-HT detection device can be developed, suitable for home health monitoring.
2. Agricultural biostimulants
5-HT is involved in stress response and growth and development regulation in plants:
Enhanced stress resistance: Exogenous application of 5-HT hydrochloride can improve crop resistance to drought, salinity, and pests, and its effect depends on the activation of 5-HT receptor analogs.
Yield improvement: In tomatoes and rice, treatment with 5-HT hydrochloride can promote fruit enlargement and grain filling, increasing yield.
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A preparation method for 5-light tryptamine hydrochloride, specifically involving the efficient synthesis of 5-light tryptamine hydrochloride through two steps of addition reaction and reduction reaction using 5-light group noise and nitroethylene as raw materials. The production of 5-light tryptamine hydrochloride by this method is a high yield, low cost, low waste, good product purity, and suitable for industrialization.
1. A preparation method for 5-light tryptamine hydrochloride, comprising the following steps:
S1: Add solvent to the reaction bottle, add 5-light base noise, add nitroethylene, and conduct a temperature rise reaction with central control tracking: after the reaction is completed, concentrate, reduce temperature and crystallize, filter, and dry the filter cake to obtain intermediate 1;
S2: Add the solvent to the high-pressure vessel, add intermediate 1, add catalyst, replace it with nitrogen, and then introduce hydrogen gas to control and track the temperature rise reaction; After the reaction is completed, filter under pressure and concentrate the filtrate to 1000: add EA to the residual solution, pass through hydrogen chloride gas, filter, wash the filter cake EA, and dry to obtain the product 5-light tryptophan hydrochloride.
2. A preparation method for 5-light tryptamine hydrochloride as claimed in claim 1, characterized in that in S1, the solvent is one of toluene and benzene.
3. A preparation method for 5-light tryptamine hydrochloride as claimed in claim 1, characterized in that the reaction temperature in S1 is between 50C and 110C.
4. A preparation method for 5-light group tryptamine hydrochloride as claimed in claim 1, characterized in that in S1, the molar ratio of 5-light group noise to nitroethylene is 1:1 to 1:3.
5. A preparation method for 5-hydroxytryptamine hydrochloride as claimed in claim 1, characterized in that the solvent in S2 is one of methanol, ethanol, isopropanol, tetrahydrofuran, or acetic acid acetic acid.
6. A preparation method for 5-light tryptamine hydrochloride as claimed in claim 1, characterized in that the reaction temperature in S2 ranges from 20C to 60C.
7. A preparation method for 5-light tryptamine hydrochloride as claimed in claim 1, characterized in that the catalyst in S2 is one of Raney nickel and Pd/C.
8. A preparation method for 5-light tryptamine hydrochloride as claimed in claim 1, characterized in that the amount of catalyst in S2 is 1% to 10% of the mass of intermediate 1.
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